Yasir Adawi

Cephalexin is a first-generation β-lactam antibiotic used in adults and pediatrics to treat various streptococcal and staphylococcal infections. This review aims to summarize and evaluate all the pharmacokinetic (PK) data on cephalexin by screening out all pertinent studies in human beings following the per oral (PO) route. By employing different online search engines such as Google Scholar, PubMed, Cochrane Central, and Science Direct, 23 studies were retrieved, among which nine were in healthy subjects, five in diseased ones, and the remaining were drug–drug, drug–food, and bioequivalence-related. These studies were included only based on the presence of plasma concentration-time profiles or PK parameters, i.e., maximum plasma concentration (C_max), half-life (t_1/2) area under the curve from time 0-infinity (AUC_0–∞), and clearance (CL/F). A dose-proportional increase in AUC_0–∞ and C_max can be portrayed in different studies conducted in the healthy population. In comparison to cefaclor, C_max was recorded to be 0.5 folds higher for cephalexin in the case of renal impairment. An increase in AUC_0–∞ was seen in cephalexin on administration with probenecid, i.e., 117 µg.h/mL vs. 68.1 µg.h/mL. Moreover, drug–drug interactions with omeprazole, ranitidine, zinc sulfate, and drug–food interactions for cephalexin and other cephalosporins have also been depicted in different studies with significant changes in all PK parameters. This current review has reported all accessible studies containing PK variables in healthy and diseased populations (renal, dental, and osteoarticular infections, continuous ambulatory peritoneal dialysis) that may be favorable for health practitioners in optimizing doses among the latter.